2. PI3K/Akt/mTOR
  3. PI3K
  4. TG100-115

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

For research use only. We do not sell to patients.

TG100-115 Chemical Structure

TG100-115 Chemical Structure

CAS No. : 677297-51-7

Size Price Stock Quantity
5 mg USD 106 In-stock
10 mg USD 172 In-stock
50 mg USD 515 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

TG100-115 Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

IC50 & Target[1]

PI3Kγ

83 nM (IC50)

PI3Kδ

235 nM (IC50)

In Vitro

TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50 values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50 values <1 μM. TG100-115 potently inhibits edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TG100-115 Related Antibodies
In Vivo

To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

346.34

Formula

C18H14N6O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=C(C(N=C2C3=CC(O)=CC=C3)=NC(N)=N1)N=C2C4=CC(O)=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (96.23 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8873 mL 14.4367 mL 28.8734 mL
5 mM 0.5775 mL 2.8873 mL 5.7747 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.22 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.22 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.01%

SDS (252 KB)

COA (250 KB) RP-HPLC (244 KB) MS (68 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/mL VEGF) in the presence or absence of test compounds (e.g., TG100-115) (10 μM), and cell numbers are quantified by XTT assay 24, 48, or 72 h later[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
Sprague-Dawley rats (175-200 g) are dosed i.v. with either TG100-115 (1 mg/kg) or vehicle, and 1-4 h later Evans blue dye is administered i.v. as 500 μl of a 2% sterile saline solution. Immediately after dye injection, animals are injected intradermally on each shaved flank with 100 μL of saline, VEGF (2 μg/mL stock), or histamine (10 μg/mL stock). Thirty minutes later, injection sites are photographed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8873 mL 14.4367 mL 28.8734 mL 72.1834 mL
5 mM 0.5775 mL 2.8873 mL 5.7747 mL 14.4367 mL
10 mM 0.2887 mL 1.4437 mL 2.8873 mL 7.2183 mL
15 mM 0.1925 mL 0.9624 mL 1.9249 mL 4.8122 mL
20 mM 0.1444 mL 0.7218 mL 1.4437 mL 3.6092 mL
25 mM 0.1155 mL 0.5775 mL 1.1549 mL 2.8873 mL
30 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4061 mL
40 mM 0.0722 mL 0.3609 mL 0.7218 mL 1.8046 mL
50 mM 0.0577 mL 0.2887 mL 0.5775 mL 1.4437 mL
60 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2031 mL
80 mM 0.0361 mL 0.1805 mL 0.3609 mL 0.9023 mL
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TG100-115 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TG100-115677297-51-7PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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